马来酸桂哌齐特的合成工艺改进

Improvement on Synthesis Process of Cinepazide Maleate

目的改进马来酸桂哌齐特的合成工艺。方法以氯乙酰氯、四氢吡咯和无水哌嗪为原料,经酰胺化、N-烷基化、酰胺化3步反应制得桂哌齐特游离碱,然后与马来酸成盐制得马来酸桂哌齐特。结果总收率为37.3%。结论本工艺操作简便,成本较低,适于工业化生产。

Objective To improve the synthesis process of cinepazide maleate.Methods Starting from chloroacetyl chloride,pyrrolidine and piperazine,cinepazide was obtained via 3 chain steps including amidation,N-alkylation and amidation.Then the salification of cinepazide with maleate yielded cinepazide maleate.Results The total yield of cinepazide maleate was 37.3%.Conclusion The improved synthesis process of cinepazide maleate can be simple,easily controlled,cost-saving and suitable for the industrial production of cinepazide maleate.